Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan, Taiwan.
Cancer Biother Radiopharm. 2009 Oct;24(5):535-41. doi: 10.1089/cbr.2008.0603.
BACKGROUND/OBJECTIVES: Intratumoral injection of a radiopharmaceutical is a potential modality to treat liver tumors. Rhenium-188 ((188)Re) was used to chelate with ethyl cysteinate dimer (ECD) in lipiodol solution to form (188)Re-ECD/lipiodol, which was then evaluated for its therapeutic potential in a rodent hepatoma model.
Male Sprague-Dawley rats were implanted with N1-S1 hepatoma cells orthotopically and randomly divided into two groups. Group 1 (n = 29) and group 2 (n = 10) received (188)Re-ECD/lipiodol (30.4 +/- 21.8 MBq/0.1 mL) and 0.1 mL of normal saline by intratumoral injection, respectively. Three rats in group 1 were imaged by micro-single-photon emission computed tomography/computed tomography scan to evaluate the biodistribution pattern. All rats were monitored for change of tumor size and survival rate after 2 months.
The in vitro stability test showed that (188)Re-ECD was well-retained in the lipiodol phase for 48 hours. The biodistribution image revealed that radioactivity was retained well in hepatomas 24 hours postinjection. Long-term studies demonstrated that rats treated with (188)Re-ECD/Lipiodol had smaller tumor volumes and a better survival rate, compared to the control group. At the end of observation, the survival rates in groups 1 and 2 were 62% and 20%, respectively (p < 0.05).
(188)Re-ECD/lipiodol via direct intratumoral injection shows potential for treating hepatoma and warrants further clinical trials.
背景/目的：瘤内注射放射性药物是治疗肝脏肿瘤的一种潜在方法。放射性核素锝-188((188)Re)与乙撑硫代氨酸二聚体(ECD)在脂质体溶液中螯合形成(188)Re-ECD/脂质体，然后在啮齿动物肝癌模型中评估其治疗潜力。
雄性 Sprague-Dawley 大鼠原位植入 N1-S1 肝癌细胞，随机分为两组。第 1 组(n=29)和第 2 组(n=10)分别经瘤内注射(188)Re-ECD/脂质体(30.4±21.8 MBq/0.1 mL)和 0.1 mL 生理盐水。第 1 组的 3 只大鼠通过微单光子发射计算机断层扫描/计算机断层扫描进行成像，以评估生物分布模式。所有大鼠在 2 个月后监测肿瘤大小变化和存活率。
体外稳定性试验表明，(188)Re-ECD 在脂质体相中 48 小时内保持良好。生物分布图像显示，注射后 24 小时放射性活性在肝癌中保留良好。长期研究表明，与对照组相比，接受(188)Re-ECD/Lipiodol 治疗的大鼠肿瘤体积较小，存活率较高。观察结束时，第 1 组和第 2 组的存活率分别为 62%和 20%(p<0.05)。
经直接瘤内注射的(188)Re-ECD/脂质体具有治疗肝癌的潜力，值得进一步临床试验。
